product name Vincristine sulfate
Description: Vincristine (also known as Leurocristine) sulfate is an inhibitor of polymerization of microtubules by binding to tubulin with IC50 of 32 μM in a cell-free assay. Vincristine is extracted from leaves of the periwinkle plant Catharanthus roseus (L.) G. Don of the family Apocynaceae. Vincristine binds irreversibly to microtubules and spindle proteins in S phase of the cell cycle and interferes with the formation of the mitotic spindle, thereby arresting tumor cells in metaphase. This agent also depolymerizes microtubules and may also interfere with amino acid, cyclic AMP, and glutathione metabolism.
References: Cancer Res. 1985 Jun;45(6):2741-7; Eur J Cancer. 1991;27(4):482-7.
923.04
Formula
C46H58N4O14S
CAS No.
2068-78-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (108.3 mM)
Water: 60 mg/mL (65.0 mM)
Ethanol: <1 mg/mL
Solubility (In vivo)
Saline: 30 mg/mL
Synonyms
Leurocristine
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19397220
| In Vitro |
In vitro activity: Vincristine inhibits net addition of tubulin dimers at assembly ends of steady-state microtubules with Ki of 85 NM. At low concentrations, Vincristine stabilizes the spindle apparatus resulting in failure of the chromosomes to segregate leading to metaphase arrest and inhibition of mitosis. At higher concentrations, Vincristine may disrupt and induce total depolymerization of microtubules. Vincristine induces apoptosis in tumor cells and inhibits SH-SY5Y cell proliferation with IC50 of 0.1 μM. Vincristine induces mitotic arrest and promots the expression of caspase-3 and -9 and cyclin B, while decreasing the expression of cyclin D. Vincristine induced neurotoxicity is caused by interference with microtubule function, which results in blockage of axonal transport and thus in axonal degeneration. Kinase Assay: Cell Assay: Cells are plated in 2 mL of medium in 35-mm plates at a concentration of about 5 × 104 cells/mL and grow for 24 h at 37 ℃ in an atmosphere of 5% CO2 and 95% air. Then medium is replaced with fresh medium lacking or containing 4 nM drug and proliferation is continued for 3 days. Cell counts are done each day in a Coulter Counter after detaching the cells with trypsin and EDTA. |
|---|---|
| In Vivo | Vincristine (3 mg/kg) administrated by a single i.p. injection to mice bearing bilateral subcutaneous xenografts Rh12 or Rh18, induces mean growth delay of >120 and >52 day, and repopulating fractions of 0.06% and 5%, respectively. Vincristine acts on subcutaneous colon 38 tumors in mice by host cell-mediated vascular effects as well as by direct tubulin-mediated cytotoxicity. Vincristine (5 mg/kg) reduces tumor blood flow of tumors by nearly 75%. |
| Animal model | Human rhabdomyosarcoma xenografts Rh12 |
| Formulation & Dosage | Dissolved in water; 3 mg/kg; i.p. injection |
| References | Cancer Res. 1985 Jun;45(6):2741-7; Eur J Cancer. 1991;27(4):482-7. |
Related Posts
product name Vincristine sulfate
Description: Vincristine (also known as Leurocristine) sulfate is an inhibitor of polymerization of microtubules by binding to tubulin with IC50 of 32 μM in a cell-free assay. Vincristine is extracted from leaves of the periwinkle plant Catharanthus roseus (L.) G. Don of the family Apocynaceae. Vincristine binds irreversibly to microtubules and spindle proteins in S phase of the cell cycle and interferes with the formation of the mitotic spindle, thereby arresting tumor cells in metaphase. This agent also depolymerizes microtubules and may also interfere with amino acid, cyclic AMP, and glutathione metabolism.
References: Cancer Res. 1985 Jun;45(6):2741-7; Eur J Cancer. 1991;27(4):482-7.
923.04
Formula
C46H58N4O14S
CAS No.
2068-78-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (108.3 mM)
Water: 60 mg/mL (65.0 mM)
Ethanol: <1 mg/mL
Solubility (In vivo)
Saline: 30 mg/mL
Synonyms
Leurocristine
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19397220
| In Vitro |
In vitro activity: Vincristine inhibits net addition of tubulin dimers at assembly ends of steady-state microtubules with Ki of 85 NM. At low concentrations, Vincristine stabilizes the spindle apparatus resulting in failure of the chromosomes to segregate leading to metaphase arrest and inhibition of mitosis. At higher concentrations, Vincristine may disrupt and induce total depolymerization of microtubules. Vincristine induces apoptosis in tumor cells and inhibits SH-SY5Y cell proliferation with IC50 of 0.1 μM. Vincristine induces mitotic arrest and promots the expression of caspase-3 and -9 and cyclin B, while decreasing the expression of cyclin D. Vincristine induced neurotoxicity is caused by interference with microtubule function, which results in blockage of axonal transport and thus in axonal degeneration. Kinase Assay: Cell Assay: Cells are plated in 2 mL of medium in 35-mm plates at a concentration of about 5 × 104 cells/mL and grow for 24 h at 37 ℃ in an atmosphere of 5% CO2 and 95% air. Then medium is replaced with fresh medium lacking or containing 4 nM drug and proliferation is continued for 3 days. Cell counts are done each day in a Coulter Counter after detaching the cells with trypsin and EDTA. |
|---|---|
| In Vivo | Vincristine (3 mg/kg) administrated by a single i.p. injection to mice bearing bilateral subcutaneous xenografts Rh12 or Rh18, induces mean growth delay of >120 and >52 day, and repopulating fractions of 0.06% and 5%, respectively. Vincristine acts on subcutaneous colon 38 tumors in mice by host cell-mediated vascular effects as well as by direct tubulin-mediated cytotoxicity. Vincristine (5 mg/kg) reduces tumor blood flow of tumors by nearly 75%. |
| Animal model | Human rhabdomyosarcoma xenografts Rh12 |
| Formulation & Dosage | Dissolved in water; 3 mg/kg; i.p. injection |
| References | Cancer Res. 1985 Jun;45(6):2741-7; Eur J Cancer. 1991;27(4):482-7. |